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An efficient synthesis of the last step key intermediate for telmisartan via Pd-catalyzed carbonylative cyclization

文献类型：期刊论文

作者Odilov, Abdullajon3,4; Qin, Hongjian2,3; Bonku, Emmanuel Mintah3,4; Zhu, Fuqiang1; Yang, Feipu4; Shen, Jingshan3,4
刊名TETRAHEDRON
出版日期2023-11-16
卷号148页码:8
关键词Telmisartan Benzimidazole Pd-catalyzed Carbonylative/cyclization
ISSN号0040-4020
DOI10.1016/j.tet.2023.133702
通讯作者Shen, Jingshan(shenjingshan@simm.ac.cn)
英文摘要The Pd-catalyzed carbonylative cyclization method is adopted for the synthesis of the penultimate intermediate of telmisartan. This highly atom-efficient reaction proceeded smoothly to provide target intermediate 1 with 87% yield under CO pressure (1 MPa) in toluene at 100 degrees C. Furthermore, the utilization of HNO3/H2SO4 in making benzimidazole 5 and polyphosphoric acid (PPA) in making bis-benzimidazole 7 in the existing processes are avoided.
WOS关键词II RECEPTOR ANTAGONISTS ; AROMATICS ; LIGANDS
资助项目Special Foundation of Chinese Academy of Sciences for strategic pilot technology[XDA12050411] ; Science and Technology Commission of Shanghai Municipality[18431907100] ; Alliance of International Science Organizations (ANSO)
WOS研究方向Chemistry
语种英语
WOS记录号WOS:001100301400001
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/307851]  
专题新药研究国家重点实验室
通讯作者Shen, Jingshan
作者单位1.Topharman Shanghai Co Ltd, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Reg, Urumqi 830011, Xinjiang, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Odilov, Abdullajon,Qin, Hongjian,Bonku, Emmanuel Mintah,et al. An efficient synthesis of the last step key intermediate for telmisartan via Pd-catalyzed carbonylative cyclization[J]. TETRAHEDRON,2023,148:8.
APA Odilov, Abdullajon,Qin, Hongjian,Bonku, Emmanuel Mintah,Zhu, Fuqiang,Yang, Feipu,&Shen, Jingshan.(2023).An efficient synthesis of the last step key intermediate for telmisartan via Pd-catalyzed carbonylative cyclization.TETRAHEDRON,148,8.
MLA Odilov, Abdullajon,et al."An efficient synthesis of the last step key intermediate for telmisartan via Pd-catalyzed carbonylative cyclization".TETRAHEDRON 148(2023):8.

入库方式： OAI收割

来源：上海药物研究所

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